EP 2690096 B1 20141126 - Process for preparation of Bendamustine
Title (en)
Process for preparation of Bendamustine
Title (de)
Verfahren zur Herstellung von Bendamustin
Title (fr)
Procédé de préparation de Bendamustine
Publication
Application
Priority
- EP 12177730 A 20120724
- EP 13163191 A 20130410
Abstract (en)
[origin: EP2690096A1] The present invention relates to a method for preparation of alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl-1 H -benzimidazol-2-yl]butanoate (7) from 2-fluoro-5-nitroaniline, comprising the steps of: a) conversion of 2-fluoro-5-nitroaniline to 5-(2-fluoro-5-nitroanilino)-5-oxopentanoic acid (1) using glutaric anhydride, conversion of compound (1) to methylammonium 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoate (2) using methylamine; conversion of compound (2) to 5-[2-(methylamino)-5-nitroanilino]-5-oxopentanoic acid (3) and condensation of compound (3) to 4-(1-methyl-5-nitro-1 H -benzimidazol-2-yl)butanoic acid (4), b) esterification of the product (4) of step a) to alkyl 4-(1-methyl-5-nitro 1H- benzimidazol-2-yl)butanoate (5), c) reduction of the product of step b) to alkyl 4-(5-amino-1-methyl- 1H -benzimidazol-2-yl)butanoate (6), and d) conversion of the product of step c) to alkyl 4-[5-[bis(2-hydroxyethyl)amino]-1-methyl- 1H -benzimidazol-2-yl]butanoate (7).
IPC 8 full level
C07D 235/16 (2006.01); A61K 31/4184 (2006.01); A61P 35/00 (2006.01)
CPC (source: EP)
A61P 35/00 (2017.12); C07D 235/16 (2013.01)
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
EP 2690096 A1 20140129; EP 2690096 B1 20141126; ES 2531616 T3 20150317
DOCDB simple family (application)
EP 13163191 A 20130410; ES 13163191 T 20130410